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- Title
Marinopyrrole Derivatives as Potential Antibiotic Agents against Methicillin-Resistant Staphylococcus aureus (III).
- Authors
Yan Liu; Haste, Nina M.; Thienphrapa, Wdee; Li, Jerry; Nizet, Victor; Hensler, Mary; Li, Rongshi
- Abstract
The marine natural product, marinopyrrole A (1), was previously shown to have significant antibiotic activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Although compound (1) exhibits a significant reduction in MRSA activity in the presence of human serum, we have identified key modifications that partially restore activity. We previously reported our discovery of a chloro-derivative of marinopyrrole A (1a) featuring a 2-4 fold improved minimum inhibitory concentration (MIC) against MRSA, significantly less susceptibility to serum inhibition and rapid and concentration-dependent killing of MRSA. Here, we report a novel fluoro-derivative of marinopyrrole A (1e) showing an improved profile of potency, less susceptibility to serum inhibition, as well as rapid and concentration-dependent killing of MRSA.
- Subjects
METHICILLIN-resistant staphylococcus aureus treatment; ANTIBIOTICS; DRUG resistance in microorganisms; MARINE pharmacology; PYRROLES
- Publication
Marine Drugs, 2014, Vol 12, Issue 9, p2458
- ISSN
1660-3397
- Publication type
Article
- DOI
10.3390/md12052458